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Compound Detail

CHEMBL4087516

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N#Cc1ccc(-c2cnccc2NS(=O)(=O)C(F)(F)F)cc1

Basic Information

ChEMBL ID CHEMBL4087516
Phase Preclinical
Structure Type MOL
InChI Key PNEHLXCEEHUQLF-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
12
PK Parameters
2
Publications
0
Known Names

Molecular Properties

327.3
MW (Da)
2.88
ALogP
4
HBA
1
HBD
82.8
PSA (Ų)
0.94
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H8F3N3O2S
MW 327.29
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -1.29

Activity Summary

IC50 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Solute carrier family 22 member 12
CHEMBL6120
IC50 8.7 8.7 2.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 6400.0 ng.hr.mL-1 Rattus norvegicus
AUC 2400.0 ng.hr.mL-1 Rattus norvegicus
CL 6.8 mL.min-1.kg-1 Rattus norvegicus
Cmax 916.62 nM Rattus norvegicus
Cmax 7944.03 nM Rattus norvegicus
F 27.0 % Rattus norvegicus
MRT 5.2 hr Rattus norvegicus
MRT 1.9 hr Rattus norvegicus
T1/2 4.4 hr Rattus norvegicus
T1/2 4.1 hr Rattus norvegicus
Tmax 0.9 hr Rattus norvegicus
Tmax 2.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28351592 10.1016/j.bmcl.2017.03.041 Rattus norvegicus 13
28351592 10.1016/j.bmcl.2017.03.041 Solute carrier family 22 member 12 1

Data from ChEMBL 36 via Core Engine